Glivec and Iressa are small-molecule tyrosine kinase inhibitors used in earlier clinical tumor therapy and have good clinical effect, which greatly stimulates interests of global leading pharmaceutical companies and research institutions in the study of such targets. Therefore, researchers have made many efforts in design, synthesis and preclinical studies of a great number of small-molecule inhibitors against many tyrosine kinase targets. Currently, many small-molecule tyrosine kinase inhibitors have been approved for clinical treatment of malignant tumors, while a number of medicaments are under clinical trials, showing broad prospects for development of such tumor-targeted molecular drugs. See, Zhang Shige, Evaluation and Analysis of Drug-Use in Hospitals of China, 2010, 10, 1: 4-6.
The pharmaceutically active compound (Z)—N-[2-(diethylamino)ethyl]-2-methyl-7-(1,2-dihydro-5-fluoro-2-oxo-3H-indol-3-ylidene)-4,5,6,7-tetrahydro-1H-indol-3-carboxamide (represented by Formula I) has significant activity in inhibition of multiple tyrosine kinases, and is capable of inhibiting proliferation of a variety of human cancer cell lines. Therefore, it can be used in preparation of anti-tumor drugs. See, Tang Feng, et al., WO2008/067756 (2008), for detailed description of biological activities of the compound and preparation thereof. The disclosures of WO2008/067756 is hereby incorporated by reference in its entirety.
